| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
GTPase Cdc42 (IC50 = 2 μM)
CASIN directly inhibits the activation of Cdc42 by binding to the Cdc42/RhoGDI complex, with an IC50 of 2 µM. By inhibiting Cdc42, it modulates cell signaling, cytoskeletal dynamics, and cell migration. |
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| ln Vitro |
CASIN (0-10 μM; 3 d) suppresses the growth of RPMI-8226/S, AMO-1, ARH-77, IM-9, JJN-3, L-363, and MOLP-8 cells[1].
CASIN (0-10 μM; 16 h) suppresses FANCD2 mono-ubiquitination induced by melphalan in LR5 cells but has no effect on S cells[1]. CASIN (5 μM; 2 d) promotes cell apoptosis in bortezomib-resistant MM patient cells[1]. In vitro, treatment with CASIN (5 µM) reduces the elevated level of active Cdc42 observed in aged primitive hematopoietic cells to the level observed in young cells. It effectively inhibits Cdc42 activity in various cell types. |
| ln Vivo |
CASIN (20 mg/kg; i.p. 2 times a day) extends the life of mice with busulfan injection[1].
In vivo, CASIN reverses the aging-related and polarity phenotype of aged hematopoietic stem cells (HSCs) to that of young HSCs. It functionally rejuvenates aged HSCs, increasing the percentage of polarized cells and restoring histone modifications. |
| Enzyme Assay |
Cell Line: AMO-1, ARH-77, IM-9 , JJN-3, L-363, MOLP-8 and RPMI-8226/S cells
Concentration: 0-10 μM Incubation Time: 3 days Result: Inhibited MM cell lines including AMO-1, ARH-77, IM-9 , JJN-3, L-363, MOLP-8 and RPMI-8226/S cells with GI50s vof 3.23, 4.31, 4.87, 2.56, 4.64, 4.67 and 3.97 μM, respectively. In vitro enzyme assays measure the direct inhibition of Cdc42 GTPase activity by CASIN. This is typically done using a GTPase activity assay, where the hydrolysis of GTP by Cdc42 is measured in the presence of the inhibitor. |
| Cell Assay |
CASIN (containing 0.02-0.2% DMSO) was used at 5 μM in the culture medium for in vitro investigations.
In vitro cell-based assays involve treating cells, such as aged HSCs or intestinal epithelial cells, with CASIN. The effect on Cdc42 activity is assessed by measuring the levels of active Cdc42 (e.g., via a pull-down assay). The impact on cell polarity, cytoskeleton organization, and phenotype is also evaluated. |
| Animal Protocol |
NSG mice with busulfan injection[3]
20 mg/kg Intraperitoneal injection; 20 mg/kg 2 times a day In vivo studies are performed in mouse models, particularly to study the effects on hematopoiesis. CASIN is administered to aged mice, and the function of HSCs is assessed by transplantation assays. The compound's ability to rejuvenate aged HSCs and improve their long-term repopulating capacity is measured. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of CASIN are not detailed in the literature. As a small molecule with activity in vivo via systemic administration, it is likely to have adequate bioavailability. It is soluble in DMSO and ethanol.
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| Toxicity/Toxicokinetics |
Toxicological data for CASIN is not available. As a research compound, it is not intended for human use. Its effects on Cdc42, a critical regulator of many cellular processes, could have significant consequences, so its use is limited to research settings.
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| References | |
| Additional Infomation |
CASIN is a valuable research tool for studying the role of Cdc42 in various biological processes, including aging, stem cell biology, and cancer. It has been shown to overcome drug resistance in multiple myeloma and facilitate the eradication of leukemia stem cells.
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| Molecular Formula |
C20H22N2O
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|---|---|
| Molecular Weight |
306.4015
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| Exact Mass |
306.173
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| Elemental Analysis |
C, 78.40; H, 7.24; N, 9.14; O, 5.22
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| CAS # |
425399-05-9
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| Related CAS # |
425399-05-9
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| PubChem CID |
2882155
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| Appearance |
Solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
577.8±50.0 °C at 760 mmHg
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| Flash Point |
303.3±30.1 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.682
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| LogP |
3.6
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
23
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| Complexity |
382
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O([H])C([H])([H])C([H])([H])N([H])C1([H])C([H])([H])C([H])([H])C([H])([H])C2C3C([H])=C(C4C([H])=C([H])C([H])=C([H])C=4[H])C([H])=C([H])C=3N([H])C1=2
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| InChi Key |
RXIUMAOXORBRCY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H22N2O/c23-12-11-21-19-8-4-7-16-17-13-15(14-5-2-1-3-6-14)9-10-18(17)22-20(16)19/h1-3,5-6,9-10,13,19,21-23H,4,7-8,11-12H2
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| Chemical Name |
2-[(6-phenyl-2,3,4,9-tetrahydro-1H-carbazol-1-yl)amino]ethanol
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| Synonyms |
CASIN
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~61 mg/mL (~199.1 mM)
Ethanol: ~61 mg/mL (~199.1 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2637 mL | 16.3185 mL | 32.6371 mL | |
| 5 mM | 0.6527 mL | 3.2637 mL | 6.5274 mL | |
| 10 mM | 0.3264 mL | 1.6319 mL | 3.2637 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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